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Suresh Pichandi et al. / Int J Cur Sci Res. 2011; 1(2): 47 - 56.
5.Lovastatin
Lovastatin is lowering cholesterol (hypolipidemic agent) in
those with hypercholesterolemia and so preventing
cardiovascular disease. Lovastatin is a naturally occurring drug
found in food such as oyster mushrooms and red yeast rice.
Lovastatin, a compound isolated from Aspergillus terreus, was the
first statin to be marketed.Lovastatin natural products with a
powerful inhibitory effect on HMG-CoA reductase,were discovered
in the 1970s, and taken into clinical development as potential
drugs for lowering LDL cholesterol. Lovastatin at its maximal
recommended dose of 80 mg daily produced a mean reduction in
LDL cholesterol of 40%, a far greater reduction than could be
obtained with any of the treatments available at the time. Equally
important, the drug produced very few adverse effects, was easy
for patients to take, and so was rapidly accepted by prescribers and
patients. Lovastatin is used for reducing total cholesterol and LDL
cholesterol, and triglycerides, and for increasing HDL cholesterol
in patients with elevated blood cholesterol levels
(hypercholesterolemia). Lovastatin is used for reducing the risk of
heart attacks,angina, coronary revascularization procedures in
individuals without symptomatic cardiovascular disease, average
to moderately elevated cholesterol levels and below average HDL
cholesterol levels. It also is used for slowing the progression of
coronary atherosclerosis in individuals with coronary heart
disease[9].
In general, lovastatin is prescribed after non-drug treatments
have not been fully successful at lowering cholesterol (e.g., diet
change, increase in exercise, weight loss if overweight). Lowering
"bad" cholesterol and triglycerides and raising "good" cholesterol
decreases the risk of heart disease and helps prevent strokes and
heart attacks. Lovastatin is usually well tolerated. Lovastatin, and
all statin drugs, can rarely cause myopathy or rhabdomyolysis.This
can be life-threatening if not recognised and treated in time, so any
unexplained muscle pain or weakness.
6.Rosuvastatin
Rosuvastatin (marketed by AstraZeneca as Crestor) is a member
of the drug class of statins,used to treat high cholesterol and
related conditions, and to prevent cardiovascular disease.
Rosuvastatin has structural similarities with most other synthetic
statins,e.g., atorvastatin,cerivastatin,pitavastatin,but rosuvastatin
unusually also contains sulfur. Rosuvastatin is a competitive
inhibitor of the enzyme HMG-CoA reductase,having a mechanism
of action similar to that of other statins.Its approximate
elimination half life is 19 hours and its time to peak plasma
concentration is reached in 3-5 hours following oral
administration.
Putative beneficial effects of rosuvastatin therapy on chronic
heart failure may be negated by increases in collagen turnover
markers as well as a reduction in plasma coenzyme Q10(CoQ10)
levels in patients with chronic heart failure.Rosuvastatin is
approved for the treatment of high LDL cholesterol (dyslipidemia)
total cholesterol (hypercholesterolemia) and/or triglycerides
(hypertriglyceridemia).In February 2010, rosuvastatin was
approved by the FDA for the primary prevention of cardiovascular
events.Rosuvastatin may decrease the relative risk of heart attack
and stroke in patients without hyperlipidemia but with elevated
levels of highly-sensitive C-reactive protein.This could strongly
impact medical practice by placing many patients on statin
prophylaxis that otherwise would have been untreated.As a result of
this clinical trial, the FDA approved rosuvastatin for the primary
prevention of cardiovascular events[10].
Low-density lipoprotein (LDL) cholesterol is the “bad”
cholesterol that increases a person's risk for cardiovascular disease
(heart problems or stroke). C-reactive protein is another substance
in the blood that serves as a marker for cardiovascular disease risk.
Statins are drugs that lower both LDL cholesterol and C-reactive
protein levels. It has been known for a long time that statins reduce
cardiovascular disease in persons with high levels of LDL
cholesterol. In 2008, a study showed that the statin rosuvastatin
reduced cardiovascular problems in persons with no previous
cardiovascular disease and normal LDL cholesterol levels but
elevated levels of C-reactive protein. The results of the initial report
of this study suggested that rosuvastatin benefited persons
regardless of their age. However, this study included larger numbers
of older persons than did many previous studies of statins and
provided an opportunity to look closely at the benefits and risks of
this statin in older persons. The most common rosuvastatin side
effects are Muscle aches or pain, Joint pain, Headache, Nausea,
Constipation, Body weakness, Abdominal pain[11].
7.Pitavastatin
Pitavastatin (usually as a calcium salt) is a member of the
medication class of statins,marketed in the United States under the
trade name Livalo. Like other statins, it is an inhibitor of HMG-CoA
reductase,the enzyme that catalyses the first step of cholesterol
synthesis. It has been available in Japan since 2003, and is being
marketed under licence in South Korea and in India. It is likely that
pitavastatin will be approved for use in hypercholesterolaemia
(elevated levels of cholesterol in the blood) and for the prevention of
cardiovascular disease outside South and Southeast Asia as
well.Like the other statins, pitavastatin is indicated for
hypercholesterolaemia (elevated cholesterol) and for the
prevention of cardiovascular disease. There have been many studies
confirming that pitavastatin can consistently increase HDL
cholesterol (10-25%), especially in patients with HDL lower than
40 mg/dl, in addition to strong reducing LDL cholesterol (-40%). As
a consequence, pitavastatin is most likely to be appropriate for
patients with metabolic syndrome with high LDL, low HDL and
diabetes mellitus.Another reason is that pitavastatin, unlike other
potent statins, does not affect glycelate control of type 2 diabetes
mellitus.[ Common statin-related side-effects (headaches, stomach
upset, abnormal liver function tests and muscle cramps) were
similar to other statins. However, pitavastatin seems to lead to less
muscle side effects than other statins. Most statins are metabolised
in part by one or more hepatic cytochrome P450 enzymes, leading